8-ethinylxanthine Derivatives as Selective A2a Receptor Antagonists

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This patent describes a new class of chemical compounds—8-ethinylxanthine derivatives—which act as highly selective antagonists for the adenosine A2A receptor. These compounds are designed to prevent or treat central nervous system diseases by blocking the A2A receptor, which is implicated in disorders such as Parkinson's disease. The invention includes specific chemical structures, methods for synthesizing these derivatives, pharmaceutical compositions containing them, and their use either alone or in combination with other therapeutic agents for neurodegenerative and movement disorders.

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• Treatment of Parkinson's disease to alleviate motor symptoms and reduce medication-induced side effects such as dyskinesia.
• Management of other central nervous system movement disorders (e.g. dystonia, catalepsy, restless legs syndrome).
• Potential treatment of neurodegenerative disorders and dementias (e.g. Alzheimer’s disease) by modulating A2A receptors.
• Adjunct therapy for migraine, pain, and possibly ischemic conditions such as stroke or cardiac ischemia through neuroprotective effects.
• Combination therapy with existing drugs like L-dopa, MAO-B inhibitors, dopamine agonists, or anticholinergics to enhance efficacy or reduce side effects in Parkinson's disease patients.

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• High affinity and selectivity for the A2A adenosine receptor, minimizing off-target effects (such as those associated with A1 receptor antagonism).
• Improved chemical stability (reduced isomerization and photosensitivity compared to previous xanthine analogues).
• Better water solubility and pharmacokinetic properties, enhancing their usability in oral or injectable formulations.
• Demonstrated effectiveness in animal models of Parkinson’s disease, showing robust activity and positive behavioral effects.
• Potential for combination therapy with other CNS drugs, providing personalized and optimized treatments.
• Broad structural diversity allows for tuning of solubility, bioavailability, and pharmacological profile, leading to more effective and safer drugs.

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Patent Abstract

The present invention relates to novel 8-ethinylxanthirtes of formula (I), pharmaceutical compositions comprising such compounds, methods for preparing such compounds and methods for using these compounds, alone or in combination with other therapeutic agents for the alleviation, prevention and/or treatment of central nervous system (CNS) diseases, disorders and conditions, such as but not limited to Parkinson's disease.